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TCPOBOP

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Chemical Structure| 76150-91-9 同义名 : -
CAS号 : 76150-91-9
货号 : A390654
分子式 : C16H8Cl4N2O2
纯度 : 97%
分子量 : 402.059
MDL号 : MFCD00057368
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(62.18 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Constitutive androstane receptor (CAR) belonging to the nuclear receptor superfamily plays an important role in the xenobiotic metabolism and disposition[1]. TCPOBOP is a mCAR agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss (EC50 = 20 nM). TCPOBOP-induced direct hyperplasia has been considered to be CAR-dependent with no evidence of involvement of cytokines or growth factor signaling[2]. Expression of CYP2B10 and CYP3A11, known CAR target genes, increased 30-fold and 45-fold, respectively, in TCPOBOP-treated mice fed the MCD diet. TCPOBOP treatment reduced hepatic steatosis (44.6 +/- 5.4% vs 30.4 +/- 4.5%, P < 0.05) and serum triglyceride levels (48 +/- 8 vs 20 +/- 1 mg/dL, P < 0.05) in MCD diet-fed mice as compared with the standard diet-fed mice. This reduction in hepatic steatosis was accompanied by an increase in enzymes involved in fatty acid microsomal omega-oxidation and peroxisomal beta-oxidation, namely CYP4A10, LPBE, and 3-ketoacyl-CoA thiolase. The reduction in steatosis was also accompanied by a reduction in liver cell apoptosis and inflammation[3]. Hepatocyte proliferation induced by TCPOBOP was associated with a stronger proliferative response and earlier S phase entry in c-jun(Δli) mice, compared to WT animals.[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.44mL

2.49mL

1.24mL

24.87mL

4.97mL

2.49mL
参考文献

[1]Suticha Kittayaruksakul,et al. Activation of constitutive androstane receptor inhibits intestinal CFTR-mediated chloride transport. Biomed Pharmacother. 2019. 111, 1249-1259.

[2]Bharat Bhushan,et al. TCPOBOP-Induced Hepatomegaly and Hepatocyte Proliferation are Attenuated by Combined Disruption of MET and EGFR Signaling. Hepatology. 2019. 69(4), 1702-1718.

[3]Edwina-S Baskin-Bey,et al. Constitutive androstane receptor agonist, TCPOBOP, attenuates steatohepatitis in the methionine choline-deficient diet-fed mouse. World J Gastroenterol. 2007. 13(42), 5635-41.

[4]Vera P Leoni,et al. Expression of c-jun is not mandatory for mouse hepatocyte proliferation induced by two nuclear receptor ligands: TCPOBOP and T3. J Hepatol. 2011. 55(5), 1069-78.